Alcohol and Sedatives Flashcards
What are the pharmacokinetics of alcohol?
-For it’s aborption, it is water and lipid soluble (does not tend to stay in the fat) and has rapid absorption in the GI tract
-The half life depends on an indivduall’s size and weight, individual metabolism rate, related food intake, and the specific beverage consumed
How does the pharmacokinetics change between gender?
-Women metabolize less ethanol than men because they have less garstic metabolism due to having less enzymes in the GI tract
-Women have less blood and muscle, while also having more fat (alcohol concentrates in plasma) due to having smaller circulatory systems and more more so alcohol stays in the fat longer
How is alcohol metabolized?
-Alcohol’s metabolism is constant over time, which means that alcohol will build and you will become progressively more drunk - the effects are additive
How does tolerance occur with alcohol?
-Tolerance occurs with chronic, heavy use and does not tend to occur in sporadic or light drinkers
What are the side effects of alcohol?
-Alcohol can cause liver damage such as hepatitis and cirrhosis, which is the cause of 75% of alcoholism death and the 12th cause of death in the US
What is a side effect of toxicity for alcohol?
Respiratory depression
What drugs are used to maintain abstinence?
-Antabuse (disulfram), Temposil - blocks metabolism and allows acetadelyde build up
-Vivitrol/Revia (naltrexone) - blocks opiod receptors, decreasing reinforcing value of alcohol
-Campral (acamprostate) - GABA agonist/glutamate NMDA antagonist
-Wellbutrin (buproprion) - DA agonist
-Serotonin agonists - SSRIs, 5-HT1A, 5-HT3, best for patients who started drinking later and less psychopathology
-Chantix (vareniciline) - nicotinic partial agonist
-Accomplia (rimonanbant) - cannabinoid antagonist
What are sedative/hypnotics?
-Hypnotics are agents that induce sleep and usually anxiolytic, but not all of them
-Most common cause of insomnia
-Consist of GABA agonists like barbiturates, non-barbiturate sedatives, BZDs, non-benzo BZRAs
What are barbiturates?
-Consist of Amytal, Alurate, Butisol, Nembutal, Luminal, Seconal, Latusate
-Half-life 10-50 hours
-Water-soluable, peak teaks occur after several hours after oral ingestion
-They have a low safety index*, high potential for dependence and abuse
What are the non-barbiturate sedatives?
-Doriden, Placidyl, Noludar, Noctect
-Most have half-lives longer than 10 hours
-Same safety/dependence issues as barbiturates
What are BZDs?
-Consist of Dalmane, Dormalin, ProSom, Restoril which have a fairly rapid onset, 12-80 hr half-life, and have active metabolites
-Also consist of Halcion, Versed, Rohypnol which have a rapid onset, 2-3hr half-life, no active metabolites, amnestic ED50 lower than somnolent ED50
-Low toxicity
What are benzodiazepines sedative/hypnotics?
-Flurazepam (Dalmane) has an onset of action of 15-45 mins and is dosed at 15-30 mg & more effective the longer you take it due to the accumulation of active metabolite with long half-life
-Triazolam (Halcion) has a short half-life and is used for short term treatment, which is best for sleep-onset insomnia
-Flunitrazepam (Rohypnol) has a 18-26 hr half-life and is an amnestic (loss of memories)
What are the nonbenzodiazepine BZRAs?
-Ambien, Sonata, Lunesta
-Low risk for dependence
-Best for sleep-onset insomnia
What is eszopiclone?
-One of the first developed medications to help treat insomnia and has been available in Europe
-If taken with a high fat/heavy meal, it can prolong onset
-Has a black box warning for potential injury or death due to complex sleep behaviors such as sleepwalking, sleep driving, and other activities
What is daridorexant?
-A dual orexin receptor antagonist used to treat insomnia in adults, it blocks the binding of wake-promoting neuropeptides of orexin
-One of the biggest side effects is CNS depression and increased thoughts of self-harm
-Has the potential to be addictive but has no research of addiction or physical dependence
-Those with narcolepsy should not take it and do not mix with alcohol
